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RU2010113933A - Алкилсульфоновые производные - Google Patents

Алкилсульфоновые производные Download PDF

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RU2010113933A
RU2010113933A RU2010113933/04A RU2010113933A RU2010113933A RU 2010113933 A RU2010113933 A RU 2010113933A RU 2010113933/04 A RU2010113933/04 A RU 2010113933/04A RU 2010113933 A RU2010113933 A RU 2010113933A RU 2010113933 A RU2010113933 A RU 2010113933A
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Хитоси ИИМОРИ (JP)
Хитоси ИИМОРИ
Хидеки КУБОТА (JP)
Хидеки КУБОТА
Сатору МИЯУТИ (JP)
Сатору МИЯУТИ
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Кайоко МОТОКИ
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Дайити Санкио Компани, Лимитед (Jp)
Дайити Санкио Компани, Лимитед
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Abstract

1. Соединение, представленное общей формулой (I) ! ! [где R1 означает С1-С6-алкильную группу, которая может иметь 1-6 атомов галогена в качестве замещающих групп, С2-С6-алкенильную группу, которая может иметь 1-6 атомов галогена в качестве замещающих групп, или С3-С7-циклоалкильную группу, которая может иметь 1-6 атомов галогена в качестве замещающих групп; ! R2 означает 6-членный, содержащий азот, ароматический моногетероцикл, имеющий 1-3 замещающие группы, или 9- или 10-членный, содержащий азот, бигетероцикл, имеющий 1-4 замещающих группы; ! Z1, Z2 и Z3 каждый независимо означает атом водорода, атом галогена или цианогруппу и ! n означает 0, 1 или 2], ! его соли или его сольваты. ! 2. Соединение по п.1, его соли или его сольваты, где R2 в общей формуле (I) является любой одной группой, выбираемой из группы, состоящей из пиридильной группы, триазолопиридильной группы и пиридопиримидинильной группы, имеющих 1-3 замещающие группы. ! 3. Соединение по п.1, его соли или его сольваты, где R2 в общей формуле (I) является пиридильной группой, имеющей 1-3 замещающие группы. ! 4. Соединение по п.1, его соли или его сольваты, где R2 в общей формуле (I) является группой, представленной следующей формулой (1) ! ! [где Ra означает атом галогена или С1-С6-алкильную группу и Rb означает карбокси-С1-С6-алкильную группу, карбамоильную группу, N-C1-C6-алкилкарбамоильную группу, N,N-ди(С1-С6-алкил)карбамоильную группу, N-(гидрокси-С1-С6-алкил)карбамоильную группу, карбоксигруппу, аминогруппу, N-(гидрокси-С1-С6-алкил)аминогруппу или С1-С6-алкилсульфониламиногруппу]. ! 5. Соединение по п.4, его соли или его сольваты, где Ra означает С1-С6-алкильную группу и Rb означает N-(гидрокси-С1-С6-алкил)карбамоильную �

Claims (20)

1. Соединение, представленное общей формулой (I)
Figure 00000001
[где R1 означает С1-С6-алкильную группу, которая может иметь 1-6 атомов галогена в качестве замещающих групп, С2-С6-алкенильную группу, которая может иметь 1-6 атомов галогена в качестве замещающих групп, или С3-С7-циклоалкильную группу, которая может иметь 1-6 атомов галогена в качестве замещающих групп;
R2 означает 6-членный, содержащий азот, ароматический моногетероцикл, имеющий 1-3 замещающие группы, или 9- или 10-членный, содержащий азот, бигетероцикл, имеющий 1-4 замещающих группы;
Z1, Z2 и Z3 каждый независимо означает атом водорода, атом галогена или цианогруппу и
n означает 0, 1 или 2],
его соли или его сольваты.
2. Соединение по п.1, его соли или его сольваты, где R2 в общей формуле (I) является любой одной группой, выбираемой из группы, состоящей из пиридильной группы, триазолопиридильной группы и пиридопиримидинильной группы, имеющих 1-3 замещающие группы.
3. Соединение по п.1, его соли или его сольваты, где R2 в общей формуле (I) является пиридильной группой, имеющей 1-3 замещающие группы.
4. Соединение по п.1, его соли или его сольваты, где R2 в общей формуле (I) является группой, представленной следующей формулой (1)
Figure 00000002
[где Ra означает атом галогена или С1-С6-алкильную группу и Rb означает карбокси-С1-С6-алкильную группу, карбамоильную группу, N-C1-C6-алкилкарбамоильную группу, N,N-ди(С1-С6-алкил)карбамоильную группу, N-(гидрокси-С1-С6-алкил)карбамоильную группу, карбоксигруппу, аминогруппу, N-(гидрокси-С1-С6-алкил)аминогруппу или С1-С6-алкилсульфониламиногруппу].
5. Соединение по п.4, его соли или его сольваты, где Ra означает С1-С6-алкильную группу и Rb означает N-(гидрокси-С1-С6-алкил)карбамоильную группу в формуле (1).
6. Соединение по п.1, его соли или его сольваты, где R2 в общей формуле (I) означает группу, представленную следующей общей формулой (2):
Figure 00000003
[где группа азотсодержащей циклической структуры представляет собой триазолопиридильную группу или пиридопиримидинильную группу; Rc означает атом галогена или С1-С6-алкильную группу; Rd означает атом водорода, гидроксигруппу, аминогруппу, N-(С1-С6-алкил)аминогруппу или N-(гидрокси-С1-С6-алкил)аминогруппу и Re означает гидроксигруппу или оксогруппу].
7. Соединение по п.1, его соли или его сольваты, где R1 в общей формуле (I) означает С1-С6-алкильную группу, которая может иметь 1-6 атомов галогена в качестве замещающих групп.
8. Соединение по п.1, его соли или его сольваты, где R1 в общей формуле (I) означает 2,2,2-трифторэтильную группу, 2-хлор-2,2-дифторэтильную группу, 2,2-дифторпропильную группу или 2,2,3,3,3-пентафторпропильную группу.
9. Соединение по п.1, его соли или его сольваты, где Z1 и Z2 оба означают атомы фтора, и Z3 означает атом водорода или Z1, Z2 и Z3 каждый означает атом фтора в общей формуле (I).
10. Соединение по п.1, его соли или его сольваты, где n в общей формуле (I) означает 2.
11. Фармацевтическая композиция, содержащая соединение по любому одному из пп.1-10, его соли или его сольваты и фармацевтически приемлемый носитель.
12. Фармацевтическая композиция по п.11 для предупреждения или лечения заболевания, связанного с аномальным генерированием и/или секрецией β-амилоидного белка.
13. Соединение по любому одному из пп.1-10, его соли или его сольваты для применения в качестве лекарственного средства.
14. Соединение по п.13, где лекарственное средство предназначено для предупреждения или лечения заболевания, связанного с аномальным генерированием и/или секрецией β-амилоидного белка.
15. Применение соединения по любому одному из пп.1-10, его солей или его сольватов для получения лекарственного средства в целях предупреждения или лечения заболевания, связанного с аномальным генерированием и/или секрецией β-амилоидного белка.
16. Способ лечения заболевания, связанного с аномальным генерированием и/или секрецией β-амилоидного белка, включающий введение эффективного количества соединения по любому одному из пп.1-10, его солей или его сольватов.
17. Фармацевтическая композиция по п.12, где заболеванием, связанным с аномальным генерированием и/или секрецией β-амилоидного белка, является болезнь Альцгеймера или синдром Дауна.
18. Соединение по п.14, где заболеванием, связанным с аномальным генерированием и/или секрецией β-амилоидного белка, является болезнь Альцгеймера или синдром Дауна.
19. Применение по п.15, где заболеванием, связанным с аномальным генерированием и/или секрецией β-амилоидного белка, является болезнь Альцгеймера или синдром Дауна.
20. Способ лечения по п.16, где заболеванием, связанным с аномальным генерированием и/или секрецией β-амилоидного белка, является болезнь Альцгеймера или синдром Дауна.
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